4-Heterocyclyl tetrahydropyridines as selective ligands for the human dopamine D 4 receptor

…, M Fielding, K Chapman, F Emms, R Marwood…

Index: Haworth; Harrison; Kulagowski; Leeson; Owens; Ridgill; Teall; Fielding; Chapman; Emms; Marwood; Patel; Moss Bioorganic and Medicinal Chemistry Letters, 1997 , vol. 7, # 17 p. 2211 - 2216

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Citation Number: 4

Abstract

A series of 1, 2, 3, 6-tetrahydropyridines 3 were synthesised, which resulted in selective high affinity dopamine D4 ligands. The SAR of heterocyclic replacements and aromatic substitution was investigated, leading to compounds of nanomolar binding affinity with excellent selectivity over both D2 and D3 receptors.